1,3-benzenediacetonitrile-α,α,{acute over (α)},{acute over (α)}-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl), 2,2′-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropiononitrile), Anastrazole, of the formula,
acts as an inhibitor of aromatase, and can be employed, either alone or in combination, for cancer therapy and prevention. Anastrozole, in particular, is widely accepted as highly effective, having only few undesirable side effects.
Preparation and purification of Anastrozole was first disclosed in EP 296,749, comprising a) the bromination of the toluene derivative, 3,5-bis(2-cyanoisopropyl)toluene, in carbon tetrachloride, producing a benzylic bromide, and b) the condensation of the resulting benzylic bromide in dimethylformamide with sodium 1,2,4-triazolyl according to the following scheme:
The desired product is then obtained after a chromatographic separation.